关键词:哒嗪酮;血小板聚集;血小板聚集抑制剂
摘 要 根据哒嗪酮类化合物的构效关系和作用机制,以CCI-17810为先导化合物,设计合成了6-〔4-(取代哌嗪基)苯基〕-5-甲基-4,5-二氢-3(2H)哒嗪酮类化合物16个.初步的体外药理试验表明:大部分目标化合物都有不同程度的抑制ADP诱导的新西兰大白兔血小板聚集作用,其中化合物(5)的活性最强,化合物(4),(6),(7)也有较强的活性,并初步探讨了其构效关系.
Synthesis and Platelet Aggregation Inhibitory Activity of
6-〔(4-Substituted-piperazinyl)phenyl〕-5-Methyl
-4,5-Dihydro-3(2H)Pyridazinones
Wu Qiuye,Ni Jin,Jiang Yuanying,Liu Chaomei
(Faculty of Pharmacy,Second Military Medicial University,Shanghai 200433)
Wu Bo,Zhang Guangming,Yao Jiayong
(Academy of Military Medicial Sciences,Beijing 100850)
Abstract Analogues of 6-〔(4-substituted-piperazine)phenyl〕-5-methyl-4,5-dihydro-3(2H)pyridazinones were synthesized in searching for more potent and selective antithrombotic drugs.All the title compounds are first reported.Results of preliminary pharmacological tests showed that all the compounds synthesized had activity against platelet aggregration induced by ADP in vitro in rabbits.Compound (5) was the most potent.Compounds (4),(6),(7)were more potent than CCI-17810 too.
Key words pyridazinones;platelet aggregation;platelet aggregation inhibitor
近年报道6-(取代苯基)-4 ......
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